PE20200527A1 - DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS - Google Patents

DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS

Info

Publication number
PE20200527A1
PE20200527A1 PE2020000001A PE2020000001A PE20200527A1 PE 20200527 A1 PE20200527 A1 PE 20200527A1 PE 2020000001 A PE2020000001 A PE 2020000001A PE 2020000001 A PE2020000001 A PE 2020000001A PE 20200527 A1 PE20200527 A1 PE 20200527A1
Authority
PE
Peru
Prior art keywords
bipirazole
derivatives
jak inhibitors
phosphate
salt
Prior art date
Application number
PE2020000001A
Other languages
Spanish (es)
Inventor
Li Yun-Long
Jincong Zhuo
Ding-Quan Qian
Song Mei
Yongchun Pan
Ganfeng Cao
Qun Li
Zhongjiang Jia
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of PE20200527A1 publication Critical patent/PE20200527A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

La presente invencion se refiere a una sal fosfato de 4-[3-(cianometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamida (compuesto 1 fosfato) de formula (i), donde la forma solida de la sal es cristalina y tiene al menos diez picos XPRD en terminos 2-theta, seleccionados de: 6.8 +/- 0.2, 7.3 +/- 0.2, 8.2 +/- 0.2, 11.1 +/- 0.2, 11.7 +/- 0.2, 12.8 +/- 0.2, 13.5 +/- 0.2, 14.7 +/- 0.2, 15.9 +/- 0.2, 16.5 +/- 0.2, 17.0 +/- 0.2, 17.3 +/- 0.2, 18.0 +/- 0.2, 18.4 +/- 0.2, entre otros. Dicho compuesto modula la actividad de la Janus quinasa (JAK), siendo util en el tratamiento de trastornos inflamatorios, trastornos autoinmunitarios, cancer, entre otros.The present invention relates to a phosphate salt of 4- [3- (cyanomethyl) -3- (3 ', 5'-dimethyl-1H, 1'H-4,4'-bipyrazol-1-yl) azetidin-1 -yl] -2,5-difluoro-N - [(1S) -2,2,2-trifluoro-1-methylethyl] benzamide (compound 1 phosphate) of formula (i), where the solid form of the salt is crystalline and has at least ten XPRD peaks in 2-theta terms, selected from: 6.8 +/- 0.2, 7.3 +/- 0.2, 8.2 +/- 0.2, 11.1 +/- 0.2, 11.7 +/- 0.2, 12.8 +/- 0.2, 13.5 +/- 0.2, 14.7 +/- 0.2, 15.9 +/- 0.2, 16.5 +/- 0.2, 17.0 +/- 0.2, 17.3 +/- 0.2, 18.0 +/- 0.2, 18.4 +/- 0.2, among others. Said compound modulates the activity of Janus kinase (JAK), being useful in the treatment of inflammatory disorders, autoimmune disorders, cancer, among others.

PE2020000001A 2013-05-17 2014-05-16 DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS PE20200527A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361824683P 2013-05-17 2013-05-17
PCT/US2014/038388 WO2014186706A1 (en) 2013-05-17 2014-05-16 Bipyrazole derivatives as jak inhibitors

Publications (1)

Publication Number Publication Date
PE20200527A1 true PE20200527A1 (en) 2020-03-09

Family

ID=50983151

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2015002406A PE20160126A1 (en) 2013-05-17 2014-05-16 DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS
PE2020000001A PE20200527A1 (en) 2013-05-17 2014-05-16 DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2015002406A PE20160126A1 (en) 2013-05-17 2014-05-16 DERIVATIVES OF BIPIRAZOLE AS JAK INHIBITORS

Country Status (35)

Country Link
US (6) US9382231B2 (en)
EP (5) EP3231801B1 (en)
JP (4) JP6415543B2 (en)
KR (3) KR102442747B1 (en)
CN (2) CN105452239B (en)
AR (2) AR096330A1 (en)
AU (5) AU2014265279B2 (en)
BR (1) BR112015028501B8 (en)
CA (1) CA2911536C (en)
CL (1) CL2015003355A1 (en)
CR (2) CR20190156A (en)
CY (3) CY1119105T1 (en)
DK (3) DK3231801T3 (en)
EA (2) EA039660B1 (en)
ES (4) ES2845210T3 (en)
FI (1) FI3786162T3 (en)
HK (2) HK1221466A1 (en)
HR (4) HRP20231048T1 (en)
HU (4) HUE033587T2 (en)
IL (4) IL242453B (en)
LT (4) LT3527263T (en)
ME (2) ME03355B (en)
MX (2) MX2015015738A (en)
MY (1) MY174788A (en)
PE (2) PE20160126A1 (en)
PH (2) PH12015502563B1 (en)
PL (3) PL3527263T3 (en)
PT (4) PT3527263T (en)
RS (4) RS56012B1 (en)
SG (2) SG11201509180WA (en)
SI (4) SI3786162T1 (en)
TR (1) TR201905814T4 (en)
TW (3) TW202116320A (en)
UA (1) UA117830C2 (en)
WO (1) WO2014186706A1 (en)

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